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BRPI0509257A - crystalline bazedoxifene acetate polymorph, composition, process for preparing a polymorph and for increasing the proportion of bazedoxifene acetate form b in a composition, methods of treating a mammal, breast cancer and a postmenopausal woman for one or more disorders vasomotor, lowering cholesterol and inhibiting bone loss in a mammal and use of a polymorph - Google Patents

crystalline bazedoxifene acetate polymorph, composition, process for preparing a polymorph and for increasing the proportion of bazedoxifene acetate form b in a composition, methods of treating a mammal, breast cancer and a postmenopausal woman for one or more disorders vasomotor, lowering cholesterol and inhibiting bone loss in a mammal and use of a polymorph

Info

Publication number
BRPI0509257A
BRPI0509257A BRPI0509257-4A BRPI0509257A BRPI0509257A BR PI0509257 A BRPI0509257 A BR PI0509257A BR PI0509257 A BRPI0509257 A BR PI0509257A BR PI0509257 A BRPI0509257 A BR PI0509257A
Authority
BR
Brazil
Prior art keywords
polymorph
mammal
composition
bazedoxifene acetate
treating
Prior art date
Application number
BRPI0509257-4A
Other languages
Portuguese (pt)
Inventor
Kadum A Ali
Pietro Allegrini
Aldo Belli
Roberto Brescello
Vincenzo Cannata
Malama K Chibwe
Livius Cotarca
Shridhar G Gangolli
Carl E Longfellow
Giorgio Soriato
Massimo Verzini
Original Assignee
Wyeth Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34965585&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0509257(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of BRPI0509257A publication Critical patent/BRPI0509257A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

POLIMORFO CRISTALINO DE ACETATO DE BAZEDOXIFENO, COMPOSIçãO, PROCESSO PARA PREPARAR UM POLIMORFO E PARA AUMENTAR A PROPORçãO DE ACETATO DE BAZEDOXIFENO FORMA BEM UMA COMPOSIçãO, MéTODOS DE TRATAR UM MAMìFERO, CáNCER DE MAMA E UMA MULHER EM PóS-MENOPAUSA PARA UM OU MAIS DISTúRBIOS VASOMOTORES, DE ABAIXAR COLESTEROL E DE INIBIR PERDA óSSEA EM UM MAMìFERO E USO DE UM POLIMORFO A presente invenção é dirigida a um polimorfo cristalino de acetato de bazedoxifeno, composições contendo o mesmo, preparações deste, e usos deste.CRYSTALLINE BAZEDOXYPHENE ACETATE POLYMORPH, COMPOSITION, PROCESS TO PREPARE A POLYMORPH AND TO INCREASE THE PROPOSAL OF BAZEDOXYPHENE ACETATE, METHODS OF TREATING A MAMPHOMUS AND A MATERIAL CANCER TO A PERSONAL MUSCHER Of lowering cholesterol and inhibiting bone loss in a mammal and use of a polymorph The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing same, preparations thereof, and uses thereof.

BRPI0509257-4A 2004-04-07 2005-04-06 crystalline bazedoxifene acetate polymorph, composition, process for preparing a polymorph and for increasing the proportion of bazedoxifene acetate form b in a composition, methods of treating a mammal, breast cancer and a postmenopausal woman for one or more disorders vasomotor, lowering cholesterol and inhibiting bone loss in a mammal and use of a polymorph BRPI0509257A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US56058404P 2004-04-07 2004-04-07
PCT/US2005/011423 WO2005100314A1 (en) 2004-04-07 2005-04-06 Crystalline polymorph of bazedoxifene acetate

Publications (1)

Publication Number Publication Date
BRPI0509257A true BRPI0509257A (en) 2007-09-11

Family

ID=34965585

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0509257-4A BRPI0509257A (en) 2004-04-07 2005-04-06 crystalline bazedoxifene acetate polymorph, composition, process for preparing a polymorph and for increasing the proportion of bazedoxifene acetate form b in a composition, methods of treating a mammal, breast cancer and a postmenopausal woman for one or more disorders vasomotor, lowering cholesterol and inhibiting bone loss in a mammal and use of a polymorph

Country Status (20)

Country Link
US (1) US7683052B2 (en)
EP (1) EP1732889A1 (en)
JP (2) JP2007532548A (en)
KR (1) KR20070004815A (en)
CN (1) CN1938271A (en)
AR (1) AR048683A1 (en)
AU (1) AU2005233114A1 (en)
BR (1) BRPI0509257A (en)
CA (1) CA2561296A1 (en)
EC (1) ECSP066910A (en)
GT (1) GT200500080A (en)
IL (1) IL178101A0 (en)
NO (1) NO20065046L (en)
PA (1) PA8629201A1 (en)
PE (1) PE20060173A1 (en)
RU (1) RU2006132352A (en)
TW (1) TW200536845A (en)
UA (1) UA86055C2 (en)
WO (1) WO2005100314A1 (en)
ZA (1) ZA200608361B (en)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR054806A1 (en) * 2005-06-29 2007-07-18 Wyeth Corp FORMULATIONS OF CONJUGATED STROGENS AND BAZEDOXIFEN
JP2009506053A (en) * 2005-08-24 2009-02-12 ワイス Bazedoxifene acetate preparation
PE20090100A1 (en) * 2007-03-30 2009-02-26 Wyeth Corp METHODS OF SEPARATION AND DETECTION OF BACEDOXIFEN ACETATE IN PHARMACEUTICAL COMPOSITIONS
CZ302358B6 (en) * 2007-07-25 2011-03-30 Zentiva, A. S. Novel crystalline salts of bazedoxifene
CA2714494A1 (en) * 2008-02-11 2009-08-20 Wyeth Llc Methods of preparing polymorphic form a of bazedoxifene acetate
WO2009102778A1 (en) * 2008-02-11 2009-08-20 Wyeth Amorphous polymorph of bazedoxifene acetate
ITMI20091109A1 (en) * 2009-06-23 2010-12-24 Wyeth Corp POLYMORPHO D FORM OF BAZEDOXIFENE ACETATE AND METHODS FOR ITS PREPARATION
CA2775599A1 (en) 2009-10-27 2011-05-12 Wyeth Llc Bazedoxifene formulations with antioxidants
WO2012007453A1 (en) 2010-07-14 2012-01-19 Sandoz Ag Crystalline compound of 1-[4-(2-azepan-1-ylethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol
EP2407467A1 (en) 2010-07-14 2012-01-18 Sandoz Ag Crystalline compound of1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol and lactic acid
US9212172B2 (en) 2010-09-14 2015-12-15 Dr. Reddy's Laboratories Limited Preparation of crystalline bazedoxifene and its salts
EP2471770A1 (en) 2010-12-28 2012-07-04 Sandoz Ag Method of preparing polymorphic pure form A of bazedoxifene acetate
CN103864664A (en) * 2012-12-18 2014-06-18 江苏柯菲平医药有限公司 Bazedoxifene acetate new crystal form and preparation method thereof
JP2016518449A (en) 2013-05-15 2016-06-23 インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションＩｎｄｉａｎａ Ｕｎｉｖｅｒｓｉｔｙ Ｒｅｓｅａｒｃｈ Ａｎｄ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏｒｐｏｒａｔｉｏｎ Processes and intermediates for preparing indole formulations
CN103864665B (en) * 2014-03-04 2016-03-02 苏州特瑞药业有限公司 The preparation method of bazedoxifene acetate
CN104030963A (en) * 2014-06-30 2014-09-10 四川大学 Preparation method of bazedoxifene acetate crystal form A
CN111004165A (en) * 2019-12-03 2020-04-14 南京正济医药研究有限公司 Preparation method of bazedoxifene acetate crystal form A
US11246874B1 (en) 2021-04-20 2022-02-15 Oxygen Biotech LLC Treatment of COVID-19

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5780497A (en) * 1996-04-19 1998-07-14 American Home Products Corporation 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents
US5880137A (en) * 1996-04-19 1999-03-09 American Home Products Corporation 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents
US5998402A (en) * 1996-04-19 1999-12-07 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
TW397821B (en) 1996-04-19 2000-07-11 American Home Produits Corp 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof
ATE206701T1 (en) 1996-04-19 2001-10-15 American Home Prod ESTROGENIC COMPOUNDS
US6005102A (en) * 1997-10-15 1999-12-21 American Home Products Corporation Aryloxy-alkyl-dialkylamines
AU757630C (en) * 1997-10-15 2006-10-26 Wyeth Novel aryloxy-alkyl-dialkylamines
US6479535B1 (en) * 1998-05-15 2002-11-12 Wyeth 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations
AR029538A1 (en) * 2000-07-06 2003-07-02 Wyeth Corp PHARMACEUTICAL COMPOSITIONS OF ESTROGEN AGENTS
EP1336602A1 (en) 2002-02-13 2003-08-20 Giovanni Scaramuzzino Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases
MXPA04012419A (en) * 2002-06-25 2005-04-19 Wyeth Corp Use of thio-oxindole derivatives in treatment of hormone-related conditions.
RU2006132180A (en) 2004-04-07 2008-05-20 Вайет (Us) CRYSTALLINE POLYMORPHAS BASEDOXIFEN ACETATE

Also Published As

Publication number Publication date
KR20070004815A (en) 2007-01-09
PA8629201A1 (en) 2005-11-25
JP2009007361A (en) 2009-01-15
AR048683A1 (en) 2006-05-17
WO2005100314A1 (en) 2005-10-27
US7683052B2 (en) 2010-03-23
ECSP066910A (en) 2006-12-20
IL178101A0 (en) 2006-12-31
RU2006132352A (en) 2008-05-20
US20050250762A1 (en) 2005-11-10
JP2007532548A (en) 2007-11-15
CN1938271A (en) 2007-03-28
NO20065046L (en) 2006-11-06
AU2005233114A1 (en) 2005-10-27
GT200500080A (en) 2005-10-31
ZA200608361B (en) 2010-03-31
CA2561296A1 (en) 2005-10-27
PE20060173A1 (en) 2006-04-12
EP1732889A1 (en) 2006-12-20
UA86055C2 (en) 2009-03-25
TW200536845A (en) 2005-11-16

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Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE AS 6A E 7A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2158 DE 15/05/2012.